透皮贴剂中药物和添加剂对压敏胶黏附性能及使用感受的影响

Effects of Drugs and Additives on Adhesion Properties and Using Feelings of Transdermal Patches

经皮给药贴剂的黏性包括初黏力、黏合力、内聚力、黏基力等,是影响患者临床使用感受的重要因素,直接关系到患者的用药依从性。本试验将《中华人民共和国药典》2015年版通则黏附力测定法中4种方法的测定结果与使用感受一一对映,考察了聚丙烯酸酯压敏胶的型号,所含有的药物、化学促透剂和增黏剂,贴剂厚度等贴剂处方因素对贴剂黏附性能的影响。结果显示,增加贴剂厚度可增加Druo-tak■87-4098型压敏胶的初黏力和黏着力,从而解决贴剂在使用时表现出的主观感受黏性不足、较易掉落的问题。加入药物富马酸比索洛尔,可通过降低黏着力改善Druo-tak■87-2510型压敏胶的拉丝现象,而加入药物阿魏酸则不能。加入增黏剂可通过增加Druo-tak■87-2510型压敏胶的内聚力而改善拉丝现象。总之,本课题将压敏胶的黏性指标与使用感受相对应,为今后贴剂处方的设计和压敏胶的选择提供参考。

The adhesion properties of transdermal patches include tack force,adhesion force,cohesive force and keying force,which are important factors affecting the using feelings of patients and are directly related to the patient compliance.The relationship between the results obtained by four methods in the general regulations of the 2015 edition of Chinese pharmacopoeia for the determination of adhesion forces and the using feelings was established,and the influences of type of polyacrylate pressure sensitive adhesive(PSA),drugs,penetration enhancers,adhesives and patch thickness on the adhesion properties were investigated.The results showed that increasing patch thickness could enhance the tack force and adhesive force of type Druo-tak■87-4098 PSA,so that it could solve the problems of poor subjective adhesive force and ease of falling off of the PSA during applying.Adding bisoprolol fumarate could improve the wire-drawing phenomenon of type Druo-tak■87-2510 PSA by reducing the adhesive force,but no obvious improvements were observed when adding ferulic acid.Differently,adding adhesives could improve the wire-drawing phenomenon of type Druo-tak■87-2510 PSA by increasing cohesive force.In conclusion,the relationship between patch adhesion properties and using feelings was established in this paper,hoping to provide some references for the design of patch formulation and the selection of PSA in future.